Syntheses of tolrestat analogs containing additional substituents in the ring and their evaluation as aldose reductase inhibitors. Identification of potent, orally active 2- …

…, J Millen, J Sredy, A Dietrich, BJ Gorham…

Index: Wrobel; Millen; Sredy; Dietrich; Gorham; Malamas; Kelly; Bauman; Harrison; Jones; Guinosso; Sestanj Journal of Medicinal Chemistry, 1991 , vol. 34, # 8 p. 2504 - 2520

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Citation Number: 27

Abstract

A series of aldose reductase inhibitors were prepared which were analogues of the potent, orally active inhibitor tolrestat (1). These compounds (5, 7, 9, and 10) have an extra substituent on one of the unoccupied positions on the naphthalene ring of 1. Primary amide prodrugs of several members from the series 5 and 7, namely 6 and 8, respectively, were also prepared. These compounds were evaluated in two in vitro systems: an isolated ...

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